细胞与分子药理学杂志

抽象的

Novel HIV Treatments by Fragment-Based Drug Design and Screening

Rosalind Franklin

Recently disulfide-rich head-to-tail cyclic peptides have attracted the hobby of medicinal chemists owing to their fantastic thermal, chemical and enzymatic steadiness added about by means of their restrained structures. Here we overview present day tendencies in the subject of peptide-based prescribed drugs and describe naturally taking place cyclic disulfide-rich peptide scaffolds, discussing their pharmaceutically beautiful houses and benefits. We describe how we can utilise these secure frameworks to graft and/or engineer pharmaceutically fascinating epitopes to amplify their selectivity and bioactivity, opening up new probabilities for addressing ‘difficult’ pharmaceutical targets. The Human Immunodeficiency Virus (HIV) is a complicated retrovirus that regularly deteriorates the immune gadget of contaminated patients, finally inflicting death. Although antiviral capsules are no longer in a position to eradicate the HIV, they are designed to inhibit the characteristic of three necessary proteins in the virus replication process: protease, reverse transcriptase and integrase. However, due to an excessive mutation rate, this virus is succesful to advance resistance to present tablets inflicting the remedy failure.